| Description | Bedaquiline (R207910) is an anti-tuberculosis drug which selectively inhibit the mycobacterial energy metabolism i.e. ATP synthesis and found to be effective against all states of Mycobacterium tuberculosis. |
| In vitro | Bedaquiline抑制TDR M. tuberculosis菌株的生长，其最小抑菌浓度（MIC）值在0.125至0.5 mg/L之间[1]。在缓慢生长的分枝杆菌（SGM）中，Bedaquiline对抗Mycobacterium avium的活性最高，其MIC50和MIC90值分别为0.03 mg/L和16 mg/L。对于快速生长的分枝杆菌（RGM），Mycobacterium abscessus subsp. abscessus（M. abscessus）和Mycobacterium abscessus subsp. massiliense（M. massiliense）对Bedaquiline的敏感性似乎高于Mycobacterium fortuitum，两种菌种的MIC50和MIC90值分别为0.13 mg/L和>16 mg/L。Bedaquiline还对非结核分枝杆菌（NTM）种显示出中等体外活性[2]。Bedaquiline对于包括耐多药的Mycobacterium tuberculosis在内的Mycobacterium tuberculosis表现出优异的体外活性[3]。 |
| Synonyms | R207910, TMC207, 贝达喹啉 |
| molecular weight | 555.5 |
| Molecular formula | C32H31BrN2O2 |
| CAS | 843663-66-1 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 5.56 mg/mL (10 mM), Sonication is recommended. |
| References | 1. Jang JC, et al. Bedaquiline susceptibility test for totally drug-resistant tuberculosis Mycobacterium tuberculosis. J Microbiol. 2017 Apr 20. 2. Pang Y, et al. In Vitro Activity of Bedaquiline against Nontuberculous Mycobacteria in China. Antimicrob Agents Chemother. 2017 Apr 24;61(5). 3. Chahine EB, et al. Bedaquiline: a novel diarylquinoline for multidrug-resistant tuberculosis. Ann Pharmacother. 2014 Jan;48(1):107-15. 4. Wang G, Dong W, Lu H, et al. Enniatin A1, A Natural Compound with Bactericidal Activity against Mycobacterium tuberculosis In Vitro[J]. Molecules. 2020, 25(1): 38. |
| Citations | 1. Briffotaux J, Xu Y, Huang W, et al. A Hydrazine–Hydrazone Adamantine Compound Shows Antimycobacterial Activity and Is a Probable Inhibitor of MmpL3. Molecules. 2022, 27(20): 7130. 2. Wang G, Dong W, Lu H, et al. Enniatin A1, A Natural Compound with Bactericidal Activity against Mycobacterium tuberculosis In Vitro. Molecules. 2020, 25(1): 38 3. Dong W, Wang G, Bai Y, et al.Repurposing an Antioxidant to Kill Mycobacterium tuberculosis by Targeting the 50S Subunit of the Ribosome.Biomolecules.2023, 13(12): 1793. |